[HTML][HTML] High-efficiency reprogramming of fibroblasts into cardiomyocytes requires suppression of pro-fibrotic signalling

Y Zhao, P Londono, Y Cao, EJ Sharpe… - Nature …, 2015 - nature.com
Y Zhao, P Londono, Y Cao, EJ Sharpe, C Proenza, R O'rourke, KL Jones, MY Jeong…
Nature communications, 2015nature.com
Direct reprogramming of fibroblasts into cardiomyocytes by forced expression of
cardiomyogenic factors, GMT (GATA4, Mef2C, Tbx5) or GHMT (GATA4, Hand2, Mef2C,
Tbx5), has recently been demonstrated, suggesting a novel therapeutic strategy for cardiac
repair. However, current approaches are inefficient. Here we demonstrate that pro-fibrotic
signalling potently antagonizes cardiac reprogramming. Remarkably, inhibition of pro-
fibrotic signalling using small molecules that target the transforming growth factor-β or Rho …
Abstract
Direct reprogramming of fibroblasts into cardiomyocytes by forced expression of cardiomyogenic factors, GMT (GATA4, Mef2C, Tbx5) or GHMT (GATA4, Hand2, Mef2C, Tbx5), has recently been demonstrated, suggesting a novel therapeutic strategy for cardiac repair. However, current approaches are inefficient. Here we demonstrate that pro-fibrotic signalling potently antagonizes cardiac reprogramming. Remarkably, inhibition of pro-fibrotic signalling using small molecules that target the transforming growth factor-β or Rho-associated kinase pathways converts embryonic fibroblasts into functional cardiomyocyte-like cells, with the efficiency up to 60%. Conversely, overactivation of these pro-fibrotic signalling networks attenuates cardiac reprogramming. Furthermore, inhibition of pro-fibrotic signalling dramatically enhances the kinetics of cardiac reprogramming, with spontaneously contracting cardiomyocytes emerging in less than 2 weeks, as opposed to 4 weeks with GHMT alone. These findings provide new insights into the molecular mechanisms underlying cardiac conversion of fibroblasts and would enhance efforts to generate cardiomyocytes for clinical applications.
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